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  • Acute intoxication  (1)
  • Key words Abecarnil  (1)
  • 1
    ISSN: 1432-1912
    Keywords: Key words Abecarnil ; Diazepam ; β-Carboline ; Anticonvulsant ; Tolerance ; Dependence ; Withdrawal ; Mice
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Development of tolerance and dependence has been reported to occur upon chronic administration of traditional benzodiazepines (BZDs). We compared the effect of chronic treatment with abecarnil, a β-carboline derivative with high affinity for central BDZ receptors, and diazepam, the BDZ prototype, in mice. After acute administration, abecarnil was as potent and effective as diazepam in protecting from bicuculline-induced convulsion. The time-course analysis of two peak equieffective doses of abecarnil (1.9 mg/kg p.o.) and diazepam (2.7 mg/kg p.o.) showed a similar duration of action. The anticonvulsant potency of diazepam was reduced in mice given chronic diazepam (25 mg/kg p.o., 2 times a day for 17 days). No tolerance to abecarnil was apparent when the drug was administered for the same period using a comparable dose (20 mg/kg p.o.). Severe symptoms of precipitated withdrawal were observed upon administration of the BDZ partial inverse agonist Ro 15–3505 in mice treated chronically with diazepam but not abecarnil. In mice made tolerant to diazepam, maximum [3H]-flumazenil binding sites were reduced in both cerebral cortex (–50%) and cerebellum (–55.2%). No changes in [3H]-flumazenil binding were measured in chronic abecarnil-treated mice. These data indicate that abecarnil possesses a very low tolerance/dependence liability and does not affect BZD receptor density after chronic administration.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Springer
    Archives of toxicology 42 (1979), S. 295-301 
    ISSN: 1432-0738
    Keywords: Isoaminile ; Compulsive abuse ; Acute intoxication ; Physical dependence test ; Cyanide release
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Zusammenfassung Isoaminil (Peracon) wurde in Italien als Drogenersatz in gewissem Umfang verwendet. Drei Beobachtungen werden berichtet. Fünf junge Leute hatten das Antitussivum in Überdosis intravenös gespritzt und zeigten schwere Symptome einer Vergiftung ähnlich wie mit Morphinderivaten. Im Tierversuch wurde festgestellt, daß Isoaminil keine Abhängigkeit erzeugte, aber Cyanid freisetzte. Allerdings waren die Mengen an Rhodanid im Urin von Ratten gering.
    Notes: Abstract Isoaminile (Peracon) has found in Italy a certain success as a substitute for hard narcotics. Three observations are reported in which five young adults have been intoxicated by the i.v. administration of the cough suppressant. On the basis of two opposed points of view suggested by the Literature to explain the compulsive abuse of this drug, the A. have studied its physical dependence capacity by using an original technique. The isoaminile cyanide release has been measured too. The experimental results demonstrate that isoaminile does not determine a physical dependence; a slight CN− release activity occurs in vivo only with high doses.
    Type of Medium: Electronic Resource
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